The present invention relates to pharmaceutical compositions for the oral administration of phloroglucinol (1,3,5-trihydroxybenzene) and to the preparation thereof. Said compositions, which are novel, are of value inasmuch as the antispasmodic activity of the phloroglucinol (antispasmodic activity on the smooth muscle fibers) is potentiated in these compositions.
Said antispasmodic activity of said phloroglucinol has been known since 1961 (reference may be made in particular to Debray et al., THERAPIE, 1961, 16, pages 978 to 990, and Cahen et al., THERAPIE, 1962, page 17). Thus phloroglucinol is used in the treatment of spasmodic and painful manifestations of the urinary tract, the hepatic ducts, the digestive tract and the gynecological apparatus. At the present time, it is administered orally in the form of tablets or lyophilizates, rectally in the form of suppositories, or by injection (i.m. or i.v.). Lyophilizates are generally preferred for oral administration in as much as they exhibit a more rapid and more complete bioavailability than tablets. Said lyophilizates are active more rapidly. The customary oral dose of phloroglucinol is generally 160 mg, taken as two tablets or lyophilizates.
In such a context, the Applicant now proposes a novel galenical form for the oral administration of said phloroglucinol. Said novel galenical form can come in a number of variants. It can be novel per se (cf., for example, the effervescent tablets, granules or powders described further in the present text) or it can consist of a modified conventional galenical form (cf., for example, the tablets or lyophilizates described further in the present text). Whatever its form of presentation, said galenical form is characteristically buffered to a pH of between 3 and 7.
According to its main subject, the present invention thus relates to pharmaceutical compositions for the oral administration of phloroglucinol, characterized in that, when liquid, they contain a system which buffers them to a pH of between 3 and 7, or in that, when solid, they contain a system which, when they are placed in an aqueous medium, is capable of exerting a buffer effect between pH 3 and pH 7.